What question did this study set out to answer?

To evaluate the receptor pharmacology, subtype selectivity, and binding characteristics of the beta-blocker and vasodilator carvedilol in human cardiac preparations.

January 1, 1992Journal of Cardiovascular Pharmacology

Receptor Pharmacology of Carvedilol in the Human Heart

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To evaluate the receptor pharmacology, subtype selectivity, and binding characteristics of the beta-blocker and vasodilator carvedilol in human cardiac preparations.
Examined carvedilol in preparations of human ventricular myocardium, myocardial membranes, and human lymphocytes containing beta-2 receptors.
Assessed competitive binding affinity (KD), beta-1 versus beta-2 receptor selectivity, alpha-1 blocking potency, and guanine nucleotide-modulatable binding.
Carvedilol exhibited high-affinity competitive beta-1 blockade with a KD of approximately 4-5 nM, a 6-fold to 39-fold selectivity for beta-1 over beta-2 receptors, and a beta-1:alpha-1 blocking relative potency of 1.7-fold.
Carvedilol demonstrated guanine nucleotide-modulatable binding in myocardial membranes and lymphocytes, but displayed no detectable intrinsic activity in isolated human heart or myocardial membrane preparations.

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Implication

In vitro study reveals carvedilol acts as a high-affinity beta- and alpha-1 blocker in human myocardium, indicating unique receptor-binding properties without intrinsic activity.

Cite This Study

Bristow et al. (1992) studied this question.

synapsesocial.com/papers/6a71631626a7f98052ddbfc3 https://doi.org/10.1097/00005344-199219001-00014

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Implication

In vitro study reveals carvedilol acts as a high-affinity beta- and alpha-1 blocker in human myocardium, indicating unique receptor-binding properties without intrinsic activity.

Receptor Pharmacology of Carvedilol in the Human Heart

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Discussion

Implication

Cite This Study

Receptor Pharmacology of Carvedilol in the Human Heart

Key Points

Discussion

Implication

Cite This Study

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